公开(公告)号：EP3115360A1

公开(公告)日：2017-01-11

申请号：EP15759282.5

申请日：2015-03-04

申请人： Zhejiang Hisun Pharmaceutical Co. Ltd.

发明人： ZHANG, Liang ,  LIU, Chuan ,  XU, Jinyi ,  ZHANG, Zhaozhao ,  CHEN, Zhi ,  CHAI, Jian ,  YANG, Zhiqing ,  LUO, Hairong ,  ZHANG, Xiangyang

IPC分类号： C07D401/12 ,  C07C303/44 ,  C07C309/04 ,  A61K31/4439 ,  A61P7/02

CPC分类号： C07D401/12 ,  C07B2200/13 ,  C07C303/44 ,  C07C309/04 ,  C07D403/12

摘要： The present invention relates to novel crystal forms M and N of dabigatran etexilate mesylate and preparation method and uses thereof, wherein the X-Ray powder diffractogram of the crystal form M has characteristic peaks at the following 2θ diffraction angles: 5.7±0.2°, 6.2±0.2°, 11.2±0.2°, 12.4±0.2°, 18.2±0.2°, 21.4±0.2°, 21.8±0.2° and 23.6±0.2°; and the X-Ray powder diffractogram of the crystal form N has characteristic peaks at the following 2θ diffraction angles: 6.0±0.2°, 11.8±0.2°, 18.2±0.2°, 21.6±0.2°, 24.4±0.2°, 27.7±0.2° and 29.7±0.2°. The crystal forms of the present invention have excellent properties in the aspects of leaching time, biological release, chemical stability and processing adaptability.

摘要翻译： 本发明涉及甲磺酸达比加群酯的新型结晶形式M和N及其制备方法和用途，其中晶型M的X射线粉末衍射图在以下2θ衍射角为5.7±0.2°处具有特征峰， 6.2±0.2°，11.2±0.2°，12.4±0.2°，18.2±0.2°，21.4±0.2°，21.8±0.2°和23.6±0.2°; 晶体形式N的X射线粉末衍射图在以下2θ衍射角处具有特征峰：6.0±0.2°，11.8±0.2°，18.2±0.2°，21.6±0.2°，24.4±0.2°，27.7± 0.2°和29.7±0.2°。 本发明的结晶形式在浸出时间，生物释放，化学稳定性和加工适应性方面具有优异的性能。